N-carbamoyl analogs of Zafirlukast:: Potent receptor antagonists of leukotriene D4

被引：6

作者：

Brown, MF ^{[1
]}

Marfat, A ^{[1
]}

Antognoli, G ^{[1
]}

Chambers, RJ ^{[1
]}

Cheng, JB ^{[1
]}

Damon, DB ^{[1
]}

Liston, TE ^{[1
]}

McGlynn, MA ^{[1
]}

O'Sullivan, SP ^{[1
]}

Owens, BS ^{[1
]}

Pillar, JS ^{[1
]}

Shirley, JT ^{[1
]}

Watson, JW ^{[1
]}

机构：

[1] Pfizer Inc, Pfizer Cent Res, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(98)00442-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Exploration of the indole nitrogen region of Zafirlukast (1) has uncovered a potent series of cysteinyl leukotriene D-4 (LTD4) antagonists. These studies showed that a variety of functionality could be incorporated in this region of the molecule without sacrificing potency. Efforts to exploit this site in order to improve oral efficacy are discussed. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：2451 / 2456

页数：6

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